U.S. Pat. No. 5,118,691 and U.S. Pat. No. 5,620,988 disclose tetrahydropyridines substituted by a quinolyl-3-alkyl radical which show a dopaminergic activity.
Dukic S. et al. (Arch. Pharm., 1997, 330 (1/2), 25–28) disclose phenylpiperidines carrying a benzimidazol-5-ylethyl substituent which also show a dopaminergic activity.
EP 164 633 discloses tetrahydropyridines substituted by a 4-indolyl radical which show an activity with regard to the central nervous system.
It has now been found that some phenyl- and pyridyltetrahydropyridines substituted by nitrogenous heterocycles have a powerful activity with regard to modulating TNF-α (Tumour Necrosis Factor).
TNF-α is a cytokine which has recently aroused interest as mediator of immunity, inflammation, cell proliferation, fibrosis, and the like. This mediator is extensively present in inflamed synovial tissue and exerts an important role in the pathogenesis of autoimmunity (Annu. Rep. Med. Chem., 1997, 32, 241–250).